KR830009022A - Method for preparing benzamido-derivatives - Google Patents

Abstract

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Description

Method for preparing benzamido-derivatives

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Claims (10)

The following methods from A to I as follows; A) by reacting the structural compound (II) with the structural compound (III) or B) N-alkylation by reacting structural compound (IV) and structural compound (V) or C) by reacting the structural compound (VI) with the structural compound (VII) or D) by reducing the structural compound (VIII) or E) reacting structural compound (IX) with protonic acid and Lewis acid to dealkylate or F) Structural compound (X) together with halogen, halogen-dioxane complex, acyl halide with Lewis acid catalysis, alkyl halide with Lewis acid catalysis, and trichloroacetonitrile, cyan halide with Lewis acid catalysis By reaction or G) by reacting the structural compound (XI) with one-step NaNO ₂ and two-step cyanide copper or halogen copper salt, or H) by reacting a structural compound (XII) with a structural compound (XIII), or I) by reacting the structural compound (XIV) with the structural compound (XV) and esterifying it, A process for preparing a salt thereof pharmacologically compatible with the following structural compound (I). T-2 In the above structural formula R ¹ and R ² are the same or different and each is a hydrogen atom, a halogen atom, a cyan group, a lower alkyl group or an acyl group R ³ is a lower alkyl group, alkenyl group, or a benzyl group substituted with fluorine, chlorine, bromine or trifluoromethyl, lower alkyl, lower alkoxy A ¹ and A ² are the same or different and each is a hydrogen atom, a lower alkyl group, an acyl group, an alkoxycarbonyl group or a dialkylcarbamyl group When A ¹ and A ² are the same lower alkyl group and R ³ is ethyl, both R ¹ and R ² are selected from cyan, lower alkyl and aryl. Z is a halogen group (chlorine, bromine) hydroxyl group X is chlorine, bromine, sulfate, phosphate, benzene sulfone salt, toluene sulfone salt Hal is chlorine, bromine R ³ 'is the same as R ³ except that there is no one carbon atom. A ^{1 '} , A ^2' is a lower alkyl group, D ¹ and D ² are the same or different and each is a hydrogen atom or an amino group When R ¹ and R ² are a halogen element or a cyan group, at least one of D ¹ and D ² is an amine group. In A'-B, A "is a lower alkyl group, B is-(SO ₄ ) _1/2 ,-(PO ₄ ) _1/3 or halogen, A ^{1 "} and A ^2" are halogen, lower alkyl group if necessary R; Alkyl, alkoxy, dialkylamino groups Z '; Chlorine, bromine. The process for producing the structural compound (I) according to claim ¹ , wherein R ¹ , R ² , and R ³ are as defined in claim ¹ , wherein one of A ¹ and A ² is a lower alkyl group, and the other is a hydrogen atom. A compound according to claim ¹ , wherein R ¹ , R ² , R ³ have the meaning given in claim ¹ , wherein one of A ¹ and A ² is lower alkyl and the other is an acyl group, alkoxycarbonyl group, or dialkyl carba Method for preparing Structural Compound (I), which is a pusher. The compound according to claim ¹ , wherein R ¹ , R ² , A ¹ and A ² are as defined in Clause 1 above, wherein R ³ is lower alkyl than alkyl, or alkenyl or fluorine, chlorine, bromine trifluoromethyl, Process for the preparation of structural compound (I) which is a benzene group substituted with lower alkyl or lower alkoxy. The process for preparing compound [-]-N-ethyl-2- (3-bromo-2-hydroxy-6-methoxybenzamidomethyl) pyrrolidine according to claim 1. The process for preparing (-)-N-ethyl-2- (3,5-dibro-2-hydroxy-6-methoxybenzamidomethyl) pyrrolidine according to claim 1. The process for preparing compound (-)-N-ethyl-2- (5-chloro-2-hydroxy-6-methoxybenzamidomethyl) pyrrolidine according to claim 1. The process for preparing compound (-)-N-ethyl-2- (3,5-diethyl-2-hydroxy-6-methoxybenzamidomethyl) pyrrolidine according to claim 1. The method according to claim 1, wherein the compound of claim 8 is used as an optical isomer. The process of claim 1 wherein the pharmacologically suitable salt of the compound of claim 1. ※ Note: The disclosure is based on the initial application.